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Assay Detail

CHEMBL1218404

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]IP3 from rat recombinant IP3R1 N-terminal residue (1-604) R36E mutant expressed in chicken DT40 cells by equilibrium competitive binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type DT40
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 (CHEMBL2804)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthetic partial agonists reveal key steps in IP3 receptor activation.
Rossi AM, Riley AM, Tovey SC, Rahman T, Dellis O, Taylor EJ, Veresov VG, Potter BV, Taylor CW.
Nat Chem Biol (2009) 5 : 631 -639
PubMed 19668195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 9.37 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1213158 1 9.40
CHEMBL279107 INS(1,4,5)P3 1 9.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1213158 Kd = 0.4 nM 9.40
CHEMBL279107 INS(1,4,5)P3 Kd = 0.46 nM 9.34